HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Potassium Carbonate → (R)-2-(4-cyano-3-(3-methylisothiazol-5-ylamino)phenylamino)-4-methylpentanamide
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Potassium Carbonate | HCID 11430 | — |
| Edukt | Binap, (A+-)- | HCID 634876 | — |
| Edukt | 3-Methylisothiazol-5-ylamine hydrochloride | HCID 2723918 | — |
| Edukt | (R)-2-(3-bromo-4-cyanophenylamino)-4-methylpentanamide | HCID 67509372 | — |
| Katalysator | palladium(II) acetate | HCID 167845 | — |
| Lösungsmittel | 1,4-Dioxane | HCID 31275 | — |
| Produkt | (R)-2-(4-cyano-3-(3-methylisothiazol-5-ylamino)phenylamino)-4-methylpentanamide | HCID 67509966 | 49,3% |
Reaktionsschritte
A mixture of (R)-2-(3-bromo-4-cyanophenylamino)-4-methylpentanamide (187 mg, 0.603 mmol), 5-amino-3-methylisothiazole hydrochloride (115 mg, 0.763 mmol), BINAP (40 mg, 0.064 mmol), Pd(OAc)2 (30 mg, 0.13 mmol) and K2CO3 (300 mg, 2.17 mmol) in dioxane (4 mL) was degassed with Ar, then was stirred at 120 C for 18 h. The mixture was concentrated in vacuo. The residue was purified by HPLC to give (R)-2-(4-cyano-3-(3-methylisothiazol-5-ylamino)phenylamino)-4-methylpentanamide (102 mg).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US08846928B2 |
| Quelldatensatz | uspto-grants-2014_09 |
| ORD ID | ord-c007ca31f92242108974824e0756c0f2 |
| Quellennotiz | uspto-grants-2014_09 |